Synthesis, characterization and biological evaluation of N-substituted triazinane-2-thiones and theoretical–experimental mechanism of condensation reaction

Sujayev A., Taslimi P., Kaya R., Safarov B., Aliyeva L., Farzaliyev V., ...Daha Fazla

Applied Organometallic Chemistry, cilt.34, sa.2, 2020 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 34 Sayı: 2
  • Basım Tarihi: 2020
  • Doi Numarası: 10.1002/aoc.5329
  • Dergi Adı: Applied Organometallic Chemistry
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, Aerospace Database, BIOSIS, Chimica, Communication Abstracts, Compendex, Metadex, DIALNET, Civil Engineering Abstracts
  • Anahtar Kelimeler: activation energy, enzyme inhibition, metabolic enzymes, N-substituted triazines, ALPHA-GLUCOSIDASE INHIBITORS, CARBONIC-ANHYDRASE, MANNICH-BASES, 1ST SYNTHESIS, ACETYLCHOLINESTERASE, BUTYRYLCHOLINESTERASE, BROMOPHENOLS, ANTIOXIDANT, DERIVATIVES, PROFILES
  • Atatürk Üniversitesi Adresli: Evet

Özet

The synthesis of triazinthions and their reactions with some nucleophilic reagents have been investigated during this scientific study. Thus, thiourea with a single component has been synthesized as a result of concomitant reactions of aldehyde and amines trials. The structure of the synthesized compounds was confirmed by H-1, C-13 NMR spectroscopy methods. The inhibitory effects of novel N-substituted triazinane-2-thione derivatives on acetylcholinesterase (AChE) activity were performed according to the spectrophotometric method of Ellman et al. These novel N-substituted triazinane-2-thiones derivatives were effective inhibitors of the alpha-glycosidase, cytosolic carbonic anhydrase I and II isoforms (hCA I and II), and Acetylcholinesterase (AChE) enzymes with K-i values in the range of 1.01 +/- 0.28 to 2.12 +/- 0.37 nm for alpha-glycosidase, 13.44 +/- 4.39 to 74.98 +/- 6.25 nm for hCA I, 10.41 +/- 4.8 to 72.6 +/- 17.66 nm for hCA II, 36.82 +/- 9.95 to 108.48 +/- 1.17 nm for AChE, and 624.62 +/- 100.34 to 1124.16 +/- 205.14 nm for alpha-glycosidase, respectively.